GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

GNE-207 (5?mg/kg) displays moderate clearance in PK. It has an acceptable oral bioavailability.

2158266-58-9

C29H30N6O3

510.59

GNE-207

DMSO:200 mg/mL (391.70 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years